LOUISVILLE, Ky.—Peptides International and Peptisyntha have
entered into a global partnership for the production of research-grade peptide
active pharmaceutical ingredients (APIs). Customers will benefit from access to
the combined research and manufacturing expertise of the two companies, as well
as seamless transition from research level through commercial manufacturing,
saving customers time and cost from peptide candidate screening through
preclinical and clinical development. The collaboration will be facilitated by
a technology transfer internal agreement.

Peptides International can produce 36 peptides in a
four-to-five day period, depending on length and sequence, running its
automated small-scale synthesizer around the clock.

In addition, Pennington notes, the company has custom
peptide synthesis expertise across a wide range of technologies, from
multi-disulfide peptides to multistep organic synthesis. PI also offers an
extensive portfolio of building blocks and other peptide synthesis tools, and
its activities have recently been certified to ISO 9001:2008 standards.

With 25 years of experience in peptide manufacturing,
Peptisyntha, a wholly owned company of Solvay, provides a seamless portfolio of
expertise from lead optimization to commercial cGMP manufacturing. Peptisyntha
has developed and demonstrated expertise in the design of cost-effective
peptide manufacturing processes and in the cGMP production of clinical and
commercial peptide APIs. Its facilities have had numerous successful U.S. Food
and Drug Administration and European Medicines Agency inspections and offer a
full range of solid-phase (SPPS), liquid-phase (LPPS) and hybrid synthesis
capabilities. With GMP manufacturing facilities in the United States and
Belgium, Peptisyntha supports all manufacturing technologies (SPPS, LPPS and
hybrid approaches) at all scales.

One reason for heightened interest in peptide chemistry is
the challenge posed by the problem of drug delivery through the cell membrane
in order to treat and manage diseases and conditions as diverse as HIV and
constipation. The discovery of cell-penetrating peptides (CPPs) represented a
major breakthrough for the transport of large-cargo molecules that may be
useful in clinical applications. CPPs are able to translocate over membranes
and gain access to the cell interior, delivering large-cargo molecules, such as
oligonucleotides, into cells.

Pennington cites a number of sulfide-bearing peptides, many
of which are derived from venom. Fuzeon (Enfuvirtide injection) is a 39-residue
peptide used in combination with other drugs to treat HIV infection in people
who have not responded well enough to other antiviral medications. Enfuvirtide
is in a class of medications called HIV fusion inhibitors. It works by stopping
HIV from infecting healthy cells.

Because chemotherapy has unwanted side effects and kills
healthy tissue around the tumor, researchers have long been interested in
developing alternative forms of therapy. The aim of targeted therapies, as the
name implies, is to target cancerous cells while leaving surrounding cells
unaffected.

One type of targeted therapy that looks promising against glioblastoma
is based on the venom of the yellow Israeli scorpion, Leiurus quinquestriatus.
The venom is among the most toxic of all scorpion venoms; it contains
histamine, enzymes, enzyme inhibitors and the potent neurotoxins chlorotoxin
and charbydotoxin, which specifically target low-conductance glioma-chloride
chloride channels (GCC) and high-conductance calcium-gated potassium channels,
respectively.

Byetta is derived from gila monster venom, Pennington notes,
and is approved to treat type 2 diabetes, both by itself and in combination
with certain oral diabetes medications. Byetta comes in an injection form and
works by increasing insulin production after meals and decreasing the amount of
sugar produced by the liver. As a result, Byetta can help lower blood sugar
levels, which can decrease the risks of developing long-term problems
associated with diabetes, including heart disease.

Finally, Linaclotide is a 15-residue peptide with three
disulfide units that can be given orally to relieve constipation, while SHK is
a potassium channel blocker derived from sea anemone toxin that is entering
clinical trials for multiple sclerosis and is a candidate for preventing
transplant rejection and in the treatment of other autoimmune diseases.